IP Library Granted Patent US 9,872,906
Granted Patent B2
US 9,872,906 · App. 14/856,075 · Granted Jan 23, 2018

Ceftolozane antibiotic compositions

Inventors: Joseph Terracciano (Concord, MA); Nicole Miller Damour (Belmont, MA); Chun Jiang (Hillsborough, CA); Giovanni Fogliato (Barzana, IT); Giuseppe Alessandro Donadelli (Casalpusterlengo, IT); Dario Resemini (Milan, IT)
Assignee: Merck Sharp & Dohme Corp.
A61K47/02A61K9/0019A61K9/19A61K31/431A61K31/546A61K47/183A61K47/12
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Quick Facts
Patent No.
US 9,872,906
App. No.
14/856,075
Granted
Jan 23, 2018
Kind
B2
Abstract

This disclosure provides pharmaceutical compositions comprising ceftolozane, pharmaceutical compositions comprising ceftolozane and tazobactam, methods of preparing those compositions, and related methods and uses of these compositions.

Claims (24)

1. A solid pharmaceutical composition comprising ceftolozane sulfate and tazobactam sodium, said composition comprising less than 0.15% of a compound of formula (III)

relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 1 month at a temperature of 25° C. and at a relative humidity of 60%, wherein the ceftolozane sulfate and tazobactam sodium provide ceftolozane active and tazobactam active in a ratio of 2:1 by weight.

2. The composition of claim 1 , which contains less than 0.1% of the compound of formula (III) relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 1 month at a temperature of 25° C. and at a relative humidity of 60%.

3. The composition of claim 1 , which contains less than 0.03% of the compound of formula (III) relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm when stored for 1 month at a temperature of 25° C. and at a relative humidity of 60%.

4. The composition of claim 1 , wherein the amount of ceftolozane active is 1,000 mg and the amount of tazobactam active is 500 mg.

5. The composition of claim 1 , wherein the amount of ceftolozane active is 2,000 mg and the amount of tazobactam active is 1,000 mg.

6. The pharmaceutical composition of claim 1 , comprising 1,147 mg ceftolozane sulfate and 537 mg tazobactam sodium.

7. The composition of claim 1 , which is provided in a unit dosage form.

8. An injectable composition comprising the pharmaceutical composition of claim 1 dissolved in a pharmaceutically acceptable vehicle.

9. A pharmaceutical composition comprising ceftolozane sulfate and tazobactam sodium, said composition comprising less than 0.15% of the compound of formula (III)

relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, and less than 1.5% of a compound of formula (IV)

relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 3 months at a temperature of 25° C. and at a relative humidity of 60%, wherein the ceftolozane sulfate and tazobactam sodium provide ceftolozane active and tazobactam active in a ratio of 2:1 by weight.

10. The composition of claim 9 , which contains less than 0.05% of the compound of formula (III) relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 3 months at a temperature of 25° C. and at a relative humidity of 60%.

11. An injectable composition comprising the pharmaceutical composition of claim 9 dissolved in a pharmaceutically acceptable vehicle.

12. A pharmaceutical composition comprising ceftolozane sulfate and tazobactam sodium, said composition comprising less than 0.15% relative to ceftolozane sulfate of the compound having a mass spectra depicted in FIG. 14 , as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 1 month at a temperature of 25° C. and at a relative humidity of 60%, wherein the ceftolozane sulfate and tazobactam sodium provide ceftolozane active and tazobactam active in a ratio of 2:1 by weight.

13. The composition of claim 12 , which contains less than 0.1% relative to ceftolozane sulfate of the compound with the mass spectra depicted in FIG. 14 , as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 1 month at a temperature of 25° C. and at a relative humidity of 60%.

14. The composition of claim 12 , which contains less than 0.03% relative to ceftolozane sulfate of the compound with the mass spectra depicted in FIG. 14 , as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 1 month at a temperature of 25° C. and at a relative humidity of 60%.

15. The composition of claim 12 , wherein the amount of ceftolozane active is 1,000 mg and the amount of tazobactam active is 500 mg.

16. The composition of claim 12 , wherein the amount of ceftolozane active is 2,000 mg and the amount of tazobactam active is 1,000 mg.

17. The pharmaceutical composition of claim 12 , comprising 1,147 mg ceftolozane sulfate and 537 mg tazobactam sodium.

18. An injectable composition comprising the pharmaceutical composition of claim 12 dissolved in a pharmaceutically acceptable vehicle.

19. A pharmaceutical composition comprising ceftolozane sulfate and tazobactam sodium, said composition comprising less than 0.15% relative to ceftolozane sulfate of a compound having a mass spectra depicted in FIG. 14 , as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, and less than 1.5% of a compound of formula (IV):

relative to ceftolozane sulfate, as determined by high performance liquid chromatography (HPLC) at a wavelength of 254 nm, when stored for 3 months at a temperature of 25° C. and at a relative humidity of 60%, wherein the ceftolozane sulfate and tazobactam sodium provide ceftolozane active and tazobactam active in a ratio of 2:1 by weight.

20. An injectable composition comprising the pharmaceutical composition claim 19 dissolved in a pharmaceutically acceptable vehicle.

Assignments (13)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 2, 2016
From: ACS DOBFAR S.P.A.
To: CUBIST PHARMACEUTICALS LLC
Reel/Frame 040492/0757 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2016
From: TERRACCIANO, JOSEPH
To: CUBIST PHARMACEUTICALS LLC
Reel/Frame 040441/0833 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2016
From: DAMOUR, NICOLE MILLER
To: CUBIST PHARMACEUTICALS LLC
Reel/Frame 040442/0029 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2016
From: JIANG, CHUN
To: CALIXA THERAPEUTICS, INC
Reel/Frame 040443/0857 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 3, 2016
From: FOGLIATO, GIOVANNI; RESEMINI, DARIO; DONADELLI, GIUSEPPE ALESSANDRO
To: ACS DOBFAR S.P.A.
Reel/Frame 040208/0741 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: DAMOUR, NICOLE MILLER
To: CUBIST PHARMACEUTICALS, INC.
Reel/Frame 039791/0136 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: JIANG, CHUN
To: CALIXA THERAPEUTICS, INC
Reel/Frame 039791/0239 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: FOGLIATO, GIOVANNI; DONADELLI, GIUSEPPE ALESSANDRO; RESEMINI, DARIO
To: ACS DOBFAR S.P.A.
Reel/Frame 039793/0151 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: ACS DOBFAR S.P.A.
To: CUBIST PHARMACEUTICALS LLC
Reel/Frame 039793/0289 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: CUBIST PHARMACEUTICALS, INC.
To: CALIXA THERAPEUTICS, INC
Reel/Frame 039793/0435 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: CALIXA THERAPEUTICS, INC
To: MERCK SHARP & DOHME CORP.
Reel/Frame 039793/0671 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 20, 2016
From: TERRACCIANO, JOSEPH
To: CUBIST PHARMACEUTICALS, INC.
Reel/Frame 039790/0927 →
Continuity (8)
Continuation In Part 14251381 · Apr 11, 2014
Continuation PCTUS2014028642 · Mar 14, 2014
Provisional Application 62051859 · Sep 17, 2014
Provisional Application 61792092 · Mar 15, 2013
Provisional Application 61793007 · Mar 15, 2013
Provisional Application 61882936 · Sep 26, 2013
Provisional Application 61893436 · Oct 21, 2013
Related Publication 20160000921A1 · Jan 7, 2016